RESUMEN
Neuropathic pain is caused by a lesion or disease of the somatosensory nervous system and has a considerable impact on the quality of life. Neuropathic pain has a dynamic and complex aetiology and gives heterogeneous symptoms across patients; therefore, it represents an important clinical challenge. Current pharmacological treatment includes tricyclic antidepressant serotonin-noradrenaline uptake inhibitors such as duloxetine, pregabalin, and gabapentin. However, these drugs do not show efficacy in all patients suffering from neuropathic pain. In this work we used a nerve chronic constriction injury mice model based on the ligation of sciatic nerve to analyse, by two-dimensional electrophoresis and mass spectrometry, blood proteins significantly altered by neuropathic pain one-week after surgery. A sham-ligated group of mice acting as control and a group of ligated mice treated with gabapentin were also analysed. The results indicated that four haptoglobin isoforms were significantly more expressed, while transthyretin and alpha-2-macroglobulin expression decreased in the serum of the murine neuropathic pain model with respect to the control mice. Interestingly, the treatment with the gabapentin reversed these conditions. The outcomes of this study can provide a further understanding of the pathophysiological meaning of the biomarkers involved in neuropathic pain.
Asunto(s)
Haptoglobinas/metabolismo , Neuralgia/sangre , Prealbúmina/metabolismo , alfa 2-Macroglobulinas Asociadas al Embarazo/metabolismo , Nervio Ciático , Animales , Biomarcadores/sangre , Modelos Animales de Enfermedad , Humanos , Masculino , Ratones , Neuralgia/tratamiento farmacológico , Inhibidores Selectivos de la Recaptación de Serotonina/farmacologíaRESUMEN
OBJECTIVES: The purpose of this work was the qualitative characterization of a recently transesterification product obtained from the coconut oil in the presence of polyglycerol-6 to produce a new PEG-free secondary surfactant. The purpose of a secondary surfactant is to reduce the harshness of a skin cleanser. METHODS: The transesterification product was qualitatively characterized in our laboratory by flow injection analysis-atmospheric pressure chemical ionization-mass spectrometry (FIA-APCI-MS). The mass spectrum of the transesterification product was compared to those of the starting materials (polyglycerol and coconut oil). RESULTS: The analyses highlighted the disappearance of the starting oil peaks and the appearance of new peaks assignable to the reaction products, mainly corresponding to diesters of polyglycerol. Additionally, peaks of unreacted polyglycerol are present as well as peaks of cyclization products derived from the polyglycerol starting material. CONCLUSIONS: The development of this fast and easy analytical method, requesting only few minutes to be performed, represents a very useful tool for the characterization of transesterification products during the quality control of batches under production.
Asunto(s)
Espectrometría de Masas/métodos , Aceites de Plantas/química , Aceite de Coco , EsterificaciónRESUMEN
Coumarin occurs in many plants used as flavoring and is known to possess hepatotoxic effects. Despite in the EFSA 'Compendium of botanicals containing toxic substances' coumarin is reported to be present in Melittis melissophyllum (bastard balm), a plant traditionally used as beverage in Italy and Serbia, to the best of our knowledge quantitative data has never been reported. Thus, the amount of coumarin in bastard balm leaves and its variation during the annual phenological cycle were determined. The subsp. melissophyllum resulted to contain high levels of coumarin (14,392 mg/kg), mainly in the early stages of the plant cycle, suggesting prudence in its use as beverage. Furthermore, coumarin was found to be useful as marker compound to differentiate the bastard balm subspecies occurring in Italy, since the subsp. albida contained a much lower content of this molecule (19-34 mg/kg).
Asunto(s)
Cumarinas/análisis , Lamiaceae/química , Bebidas , Cromatografía Líquida de Alta Presión , Cumarinas/toxicidad , Italia , Lamiaceae/clasificación , Lamiaceae/toxicidad , Hojas de la Planta/química , Especificidad de la EspecieRESUMEN
Eight taxa of the Hypericum spp. growing in Central Italy (Appennino Umbro-Marchigiano) were analyzed by HPLC-DAD for constituents quantitation, for antioxidant and free radical scavenging activities. H. perforatum subsp. veronense was the richest in phenolic compounds and hyperforin was detected for the first time in H. hircinum subsp. majus. Significant values of antioxidant activity were found in the investigated Hypericum taxa.
Asunto(s)
Antioxidantes/farmacología , Hypericum , Fitoterapia , Extractos Vegetales/farmacología , Antioxidantes/administración & dosificación , Antioxidantes/química , Antioxidantes/uso terapéutico , Compuestos de Bifenilo , Humanos , Italia , Peroxidación de Lípido/efectos de los fármacos , Medicina Tradicional , Fenoles/administración & dosificación , Fenoles/química , Fenoles/farmacología , Fenoles/uso terapéutico , Picratos/química , Componentes Aéreos de las Plantas , Extractos Vegetales/administración & dosificación , Extractos Vegetales/química , Extractos Vegetales/uso terapéuticoRESUMEN
Eight entities of the genus Hypericum that spontaneously grow on the Central Italy (Appennino Umbro-Marchigiano) have been studied under the morphological, histochemical and phytochemical aspects. From the morphological standpoint, they differ in the shape and size of flowers and leaves and in the dimension and distribution of the secretory structures through the various parts of the plant. It has been possible, with the histochemical and phytochemical studies, to localize and identify some secondary metabolites inside the secretory structures.
Asunto(s)
Hypericum/anatomía & histología , Hypericum/clasificación , Fitoterapia , Humanos , Hypericum/metabolismo , Italia , Medicina TradicionalRESUMEN
A series of dimeric derivatives (+)-1, and (+)-2, and (+)-3a-d of L-Dopa diacetyl esters was synthesized and evaluated as potential L-Dopa prodrugs with improved physicochemical properties. All the new compounds showed chemical stability in aqueous buffer solutions (pH 1.3 and 7.4). A relatively slow release of L-Dopa in human plasma was observed.
Asunto(s)
Levodopa/síntesis química , Levodopa/farmacocinética , Profármacos/síntesis química , Profármacos/farmacocinética , Animales , Dimerización , Estabilidad de Medicamentos , Semivida , Humanos , Concentración de Iones de Hidrógeno , Hidrólisis , Levodopa/análogos & derivados , Plasma/metabolismo , RatasRESUMEN
The synthesis and in vitro chemical and enzymatic stability of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine (9) as L-Dopa prodrug are described. Prodrug 9 possesses a good lipophilicity (log P = 2.153 +/- 0.017), is stable in aqueous buffer solutions (pH 1.3 and 7.4), and in 80% rat and human plasma it is turned into L-Dopa.